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Drug Delivery

Kaiping Wang, Fang Cheng, Xianglin Pan, Tao Zhou, Xiqiu Liu, Ziming Zheng, Li Luo, Yu Zhang
To investigate the absorption and delivery of ASP in gastrointestinal (GI) tract, cASP was successfully synthesized by chemically modifying with succinic anhydride and then conjugating with a near infrared fluorescent dye Cy5.5. Then, the capacity of oral absorption of cASP was evaluated. The results demonstrated that cASP had low toxicity and no disruption on the integrity of cell membrane. The endocytosis of cASP into the epithelial cells was time- and energy-dependent, which was mediated by macropinocytosis pathway and clathrin- and caveolae (or lipid raft)-related routes...
November 2017: Drug Delivery
Liling Mei, Jintian Chen, Siqin Yu, Ying Huang, Yecheng Xie, Hui Wang, Xin Pan, Chuanbin Wu
Vaginal delivery of antimicrobial drugs is the most effective method for the local treatment of the vaginal infections. However, current vaginal drug delivery systems (VDDS), including gel, lotion, aerosol and cream, are suffering from low penetration in the deep vaginal rugae and easy elimination by self-cleaning of vaginal canal. To address these issues, a foam aerosol based on the thermal transformation was designed to improve penetration efficiency and achieve the extended retention. The expansible thermal gelling foam aerosol (ETGFA) consisting of thermal sensitive matrix, silver nanoparticle, adhesive agent and propellant, was optimized by evaluations of precursor viscosity, foam expansion, thermal gelation, gel adhesiveness, antimicrobial effects and tissue irritation...
November 2017: Drug Delivery
Sen Yao, Xuqian Li, Jingxuan Liu, Yuqing Sun, Zhuanhe Wang, Yanyan Jiang
Mesenchymal stem cells (MSCs), exhibiting tumor-tropic and migratory potential, can serve as cellular carriers to improve the effectiveness of anticancer agents. However, several challenges, such as the safety issue, the limited drug loading, the conservation of stemness and migration of MSCs, still remain in the MSC-based delivery system. In the present study, a novel nano-engineered MSC delivery system was established by loading doxorubicin (DOX)-polymer conjugates for the systemic treatment of pulmonary metastasis of breast cancer...
November 2017: Drug Delivery
Shiva Pathak, Shobha Regmi, Biki Gupta, Bijay K Poudel, Tung Thanh Pham, Chul Soon Yong, Jong Oh Kim, Jae-Ryong Kim, Min Hui Park, Young Kyung Bae, Simmyung Yook, Cheol-Hee Ahn, Jee-Heon Jeong
Immune rejection after transplantation is common, which leads to prompt failure of the graft. Therefore, to prolong the survival time of the graft, immunosuppressive therapy is the norm. Here, we report a robust immune protection protocol using FK506-loaded microspheres (FK506M) in injectable hydrogel. Pancreatic islets were codelivered with the FK506M into the subcutaneous space of streptozocin-induced diabetic mice. The islets codelivered with 10 mg/kg FK506M maintained normal blood glucose levels during the study period (survival rate: 60%)...
November 2017: Drug Delivery
Longfa Kou, Qing Yao, Sathish Sivaprakasam, Qiuhua Luo, Yinghua Sun, Qiang Fu, Zhonggui He, Jin Sun, Vadivel Ganapathy
l-Carnitine, obligatory for oxidation of fatty acids, is transported into cells by the Na(+)-coupled transporter OCTN2 and the Na(+)/Cl(-)-coupled transporter ATB(0,+). Here we investigated the potential of L-carnitine-conjugated poly(lactic-co-glycolic acid) (PLGA) nanoparticles (LC-PLGA NPs) to deliver chemotherapeutic drugs into cancer cells by targeting the nanoparticles to both OCTN2 and ATB(0,+). The cellular uptake of LC-PLGA NPs in the breast cancer cell line MCF7 and the colon cancer cell line Caco-2 was increased compared to unmodified nanoparticles, but decreased in the absence of co-transporting ions (Na(+) and/or Cl(-)) or in the presence of competitive substrates for the two transporters...
November 2017: Drug Delivery
Daniel J Denmark, Robert H Hyde, Charlotte Gladney, Manh-Huong Phan, Kirpal S Bisht, Hariharan Srikanth, Pritish Mukherjee, Sarath Witanachchi
Conventional therapeutic techniques treat patients by delivering biotherapeutics to the entire body. With targeted delivery, biotherapeutics are transported to the afflicted tissue reducing exposure to healthy tissue. Targeted delivery devices are minimally composed of a stimuli responsive polymer allowing triggered release and magnetic nanoparticles enabling targeting as well as alternating magnetic field (AMF) heating. Although more traditional methods, like emulsion polymerization, have been used to realize such devices, the synthesis is problematic...
November 2017: Drug Delivery
Hao Dong, Li Tian, Meng Gao, Hong Xu, Chenghong Zhang, Li Lv, Jianbin Zhang, Changyuan Wang, Yan Tian, Xiaochi Ma
Liver cancer is one of the major diseases affecting human health. Modified drug delivery systems through the asialoglycoprotein receptor, which is highly expressed on the surface of hepatocytes, have become a research focus for the treatment of liver cancer. Resibufogenin (RBG) is a popular traditional Chinese medicine and natural anti-cancer drug that was isolated from Chansu, but its cardiotoxicity and hydrophobicity have limited its clinical applications. Galactosyl-succinyl-poloxamer 188 and galactosyl-succinyl-poloxamer 188-polylactide-co-glycolide (Gal-SP188-PLGA) were synthesized using galactose, P188, and PLGA to achieve active liver-targeting properties...
November 2017: Drug Delivery
Xinyi Li, Yuan Yang, Yiping Jia, Xuan Pu, Ting Yang, Yicheng Wang, Xuefei Ma, Qi Chen, Mengwen Sun, Dapeng Wei, Yu Kuang, Yang Li, Yu Liu
BACKGROUND: Multifunctional magnetic nanoparticles (MNP) have been newly developed for tumor-targeted drug carriers. To address challenges including biocompatibility, stability, nontoxicity, and targeting efficiency, here we report the novel drug deliverer poly(ethylene glycol) carboxyl-poly(ɛ-caprolactone) modified MNP (PEG-PCCL-MNP) suitable for magnetic targeting based on our previous studies. METHODS: Their in vitro characterization and cytotoxicity assessments, in vivo cytotoxicity assessments, and antitumor efficacy study were elaborately investigated...
November 2017: Drug Delivery
Thiruganesh Ramasamy, Pasupathi Sundaramoorthy, Hima Bindu Ruttala, Yongjoo Choi, Woo Hyun Shin, Jee-Heon Jeong, Sae Kwang Ku, Han-Gon Choi, Hwan Mook Kim, Chul Soon Yong, Jong Oh Kim
Since breast cancer is one of the most lethal malignancies, targeted strategies are urgently needed. In this study, we report the enhanced therapeutic efficacy of docetaxel (DTX) when combined with polyunsaturated fatty acids (PUFA) for effective treatment of multi-resistant breast cancers. Folic acid (FA)-conjugated PUFA-based lipid nanoparticles (FA-PLN/DTX) was developed. The physicochemical properties, in vitro uptake, in vitro cytotoxicity, and in vivo anticancer activity of FA-PLN/DTX were evaluated. FA-PLN/DTX could efficiently target and treat human breast tumor xenografts in vivo...
November 2017: Drug Delivery
Yue Hu, Zhou Chen, He Zhang, Mingkai Li, Zheng Hou, Xiaoxing Luo, Xiaoyan Xue
Nanocarriers of drugs have attracted significant attention to tackle the problems of drug resistance or nucleic acid drug delivery, which can optimize pharmaceutical parameters and enhance the cellular uptake efficiency. Nowadays, DNA nanostructure presents an opportunity in the field of nanomaterial due to its precise control in shape and size, excellent biocompatibility, as well as multiple sites for targeting decoration. DNA tetrahedron, which is stable and easily synthesized, is used for various applications, including nuclear magnetic resonance imaging, molecular diagnosis, targeting drug delivery, and so on...
November 2017: Drug Delivery
Ye Tao, Yue Wang, Zhao Ma, Liqiang Wang, Limin Qin, Lu Wang, Yi Fei Huang, Shizhong Zhang
Retinitis pigmentosa (RP) is a heterogeneous group hereditary retinal disease that is characterized by photoreceptor degeneration. The present study sought to explore the therapeutic effects of erythropoietin (EPO) on the N-methyl-N-nitrosourea (MNU)-induced photoreceptor degeneration. The MNU-administered mouse or normal control received a subretinal injection of EPO (at the dose of 10U). Twenty-four hours after EPO injection, the retinal EPO levels of experimental animals were quantified. Subsequently, the experimental animals were subjected to optokinetic tests, ERG examination, SD-OCT examination, histology assessment, and immunohistochemistry evaluation...
November 2017: Drug Delivery
Leila Farahmand, Behrad Darvishi, Keivan Majidzadeh-A
As a prototypical pro-inflammatory transcription factor, constitutive activation of NF-κB signaling pathway has been reported in several chronic inflammatory disorders including inflammatory bowel disease, cystic fibrosis, rheumatoid arthritis and cancer. Application of decoy oligodeoxynucleotides (ODNs) against NF-κB, as an effective molecular therapy approach, has brought about several promising outcomes in treatment of chronic inflammatory disorders. However, systematic administration of these genetic constructs is mostly hampered due to their instability, rapid degradation by nucleases and poor cellular uptake...
November 2017: Drug Delivery
Min Zhou, Xin Li, Yuanyuan Li, Qiu'e Yao, Yue Ming, Ziwei Li, Laichun Lu, Sanjun Shi
A co-loaded drug delivery system based on ascorbyl palmitate that can transport various functional drugs to their targets within a tumor represents an attractive strategy for increasing the efficiency of anticancer treatment. In this study, we developed a dual drug delivery system to encapsulate ascorbyl palmitate (AP) and paclitaxel (PTX) for synergistic cancer therapy. AP, which is a vitamin C derivative, and PTX were incorporated into solid lipid nanoparticles (AP/PTX-SLNs), which were used to treat murine B16F10 melanoma that had metastasized to the lungs of mice...
November 2017: Drug Delivery
Mine Orlu, Sejal R Ranmal, Yucheng Sheng, Catherine Tuleu, Paul Seddon
Orodispersible films (ODFs) possess potential to facilitate oral drug delivery to children; however, documentation of their acceptability in this age group is lacking. This study is the first to explore the initial perceptions, acceptability and ease of use of ODFs for infants and preschool children, and their caregivers through observed administration of the type of dosage form. Placebo ODFs were administered to children stratified into aged 6 to 12 months, 1 year, 2 years, 3 years, 4 years and 5 years old and into those with an acute illness or long-term stable condition in hospital setting...
November 2017: Drug Delivery
Haibin Wu, Meng Wang, Bo Dai, Yanmin Zhang, Ying Yang, Qiao Li, Mingyue Duan, Xi Zhang, Xiaomei Wang, Anmao Li, Liyu Zhang
Since conventional chemotherapy for acute myeloid leukemia (AML) has its limitations, a theranostic platform with targeted and efficient drug transport is in demand. In this study, we developed the first CD123 (AML tumor marker) aptamers and designed a novel CD123-aptamer-mediated targeted drug train (TDT) with effective, economical, biocompatible and high drug-loading capacity. These two CD123 aptamers (termed as ZW25 and CY30, respectively) can bind to a CD123 peptide epitope and CD123 + AML cells with high specificities and KD of 29...
November 2017: Drug Delivery
Ki-Taek Kim, Joon Lee, Min-Hwan Kim, Ju-Hwan Park, Jae-Young Lee, Joo-Hyun Song, Minwoong Jung, Myoung-Hoon Jang, Hyun-Jong Cho, In-Soo Yoon, Dae-Duk Kim
Topical and transdermal drug delivery has great potential in non-invasive and non-oral administration of poorly bioavailable therapeutic agents. However, due to the barrier function of the stratum corneum, the drugs that can be clinically feasible candidates for topical and transdermal delivery have been limited to small-sized lipophilic molecules. Previously, we fabricated a novel iontophoretic system using reverse electrodialysis (RED) technology (RED system). However, no study has demonstrated its utility in topical and/or transdermal delivery of poorly permeable therapeutic agents...
November 2017: Drug Delivery
Rui Chen, Liu Xu, Qin Fan, Man Li, Jingjing Wang, Li Wu, Weidong Li, Jinao Duan, Zhipeng Chen
Inhalation administration, compared with intravenous administration, significantly enhances chemotherapeutic drug exposure to the lung tissue and may increase the therapeutic effect for pulmonary anticancer. However, further identification of cancer cells after lung deposition of inhaled drugs is necessary to avoid side effects on normal lung tissue and to maximize drug efficacy. Moreover, as the action site of the major drug was intracellular organelles, drug target to the specific organelle is the final key for accurate drug delivery...
November 2017: Drug Delivery
Ding Qu, Mengfei Guo, Yue Qin, Lixiang Wang, Bing Zong, Yunyan Chen, Yan Chen
Previously, we have developed a multicomponent-based microemulsion composed of etoposide, coix seed oil, and ginsenoside Rh2 (ECG-MEs). In this study, our goal was to validate the feasibility of ECG-MEs in lung cancer treatment and explore the mechanism underling the enhanced antitumor efficacy. The optimal weight ratio of ginsenoside Rh2 (G-Rh2) in ECG-MEs was determined as 3% (wt%), that was capable of forming the microemulsion readily with small particle size and high drug encapsulation efficiency. In cellular studies, the intracellular fluorescence of human non-small cell lung cancer (A549) cells treated with fluorescein isothiocyanate-labeled ECG-MEs (FITC/ECG-MEs) was significantly higher than that of various controls, leading to the obviously synergistic anticancer activities in cytotoxicity and in vitro cell apoptosis induction...
November 2017: Drug Delivery
Huiyun Zhang, Wenqian Xu, Emmanuel Omari-Siaw, Yingkun Liu, Baoding Chen, Deyu Chen, Jiangnan Yu, Ximing Xu
Periplocymarin (PPM), a cardiac glycoside, has a narrow therapeutic index, poor tumor selectivity and severe cardiovascular toxicity which hinder its wide clinical applications in cancer treatment. Herein, we report novel redox-responsive prodrug-nanoparticles (MPSSV-NPs) self-assembled by co-nanoprecipitation of PPM-vitamin E conjugate and a PEG derivative of linoleate (mPEG2000-LA) in water. It was found that the characteristics of PPM-vitamin E nanoparticles (PSSV-NPs) were improved through co-nanoprecipitation with increased percentages of mPEG2000-LA...
November 2017: Drug Delivery
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